Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

Kanchan Devkota; Brian Lohse; Qing Liu; Ming-Wei Wang; Dan Stærk; Jens Berthelsen; Rasmus Prætorius Clausen

doi:10.1021/ml4002503

Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

Kanchan Devkota, Brian Lohse, Qing Liu, Ming-Wei Wang, Dan Stærk, Jens Berthelsen, Rasmus Prætorius Clausen

28 Citations (Scopus)

Abstract

A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.

Original language	English
Journal	A C S Medicinal Chemistry Letters
Volume	5
Issue number	4
Pages (from-to)	293-297
ISSN	1948-5875
DOIs	https://doi.org/10.1021/ml4002503
Publication status	Published - 10 Apr 2014

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title = "Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2",

abstract = "A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.",

author = "Kanchan Devkota and Brian Lohse and Qing Liu and Ming-Wei Wang and Dan St{\ae}rk and Jens Berthelsen and Clausen, {Rasmus Pr{\ae}torius}",

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T1 - Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

AU - Devkota, Kanchan

AU - Lohse, Brian

AU - Liu, Qing

AU - Wang, Ming-Wei

AU - Stærk, Dan

AU - Berthelsen, Jens

AU - Clausen, Rasmus Prætorius

PY - 2014/4/10

Y1 - 2014/4/10

N2 - A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.

AB - A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.

U2 - 10.1021/ml4002503

DO - 10.1021/ml4002503

M3 - Letter

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SN - 1948-5875

VL - 5

SP - 293

EP - 297

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 4

ER -

Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

Abstract

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